CWHM-1552 是一种口服有效的恶性疟原虫抑制剂，对 3D7 和 Dd2 strain 的 IC50s 分别是 51 nM and 53 nM。
CWHM-1552 is an orally efficacious inhibitor of P. falciparum with IC50s of 51 nM and 53 nM for 3D7 and Dd2 strain, respectively[1]. IC50: 51 nM (3D7 strain) and 53 nM (Dd2 strain)[1]
CWHM-1552 (Compound (-)-32a) (orally; 3-30 mg/kg/day for 4 days) inhibits parasitemia at 99.9% at 30 mg/kg/day and 94% at 10 mg/kg/day[1]. CWHM-1552 (i.v. administration; 2 mg/kg/day for 48 hours) has respectable half-lives (2.7 h) and low clearance in mice[1]. CWHM-1552 has good pharmacokinetic properties and oral efficacy in a mouse model of malaria. CWHM-1552 has an in vivo ED90 of P. chabaudi ASS infected Mice[1]
[1]. Meyers MJ, et al. 4-Aryl Pyrrolidines as Novel Orally Efficacious Antimalarial Agents. Part 2: 2-Aryl-N-(4-arylpyrrolidin-3-yl) acetamides. ACS Med Chem Lett. 2019 May, 10(6):966-971.
动态评分
0.0